SK14699A3 - Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides - Google Patents

Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides Download PDF

Info

Publication number: SK14699A3
Authority: SK; Slovakia
Prior art keywords: group; compound; aspartyl; butanoyl; piperidin
Prior art date: 1996-08-21

Application number

SK146-99A

Other languages

English (en)

Slovak (sk)

Inventor

Scott I Klein

Bruce F Molino

Mark Czekaj

Charles J Gardner

Original Assignee

Rhone Poulenc Rorer Pharma

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1996-08-21

Filing date

1997-08-15

Publication date

2000-11-07

1997-08-15 Application filed by Rhone Poulenc Rorer Pharma filed Critical Rhone Poulenc Rorer Pharma

2000-11-07 Publication of SK14699A3 publication Critical patent/SK14699A3/sk

Links

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150000001875 compounds Chemical class 0.000 claims abstract description 101
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IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
125000000753 cycloalkyl group Chemical group 0.000 claims description 24
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229920006395 saturated elastomer Polymers 0.000 description 1
239000012047 saturated solution Substances 0.000 description 1
238000013391 scatchard analysis Methods 0.000 description 1
229960001153 serine Drugs 0.000 description 1
239000008159 sesame oil Substances 0.000 description 1
235000011803 sesame oil Nutrition 0.000 description 1
239000000741 silica gel Substances 0.000 description 1
229910002027 silica gel Inorganic materials 0.000 description 1
239000000377 silicon dioxide Substances 0.000 description 1
239000012312 sodium hydride Substances 0.000 description 1
229910000104 sodium hydride Inorganic materials 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
239000006104 solid solution Substances 0.000 description 1
230000003595 spectral effect Effects 0.000 description 1
238000010183 spectrum analysis Methods 0.000 description 1
230000000087 stabilizing effect Effects 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
239000008107 starch Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
238000003860 storage Methods 0.000 description 1
238000010254 subcutaneous injection Methods 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
150000003890 succinate salts Chemical class 0.000 description 1
IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid Chemical class NS(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 description 1
229910052717 sulfur Inorganic materials 0.000 description 1
239000011593 sulfur Substances 0.000 description 1
150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
235000020357 syrup Nutrition 0.000 description 1
239000006188 syrup Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
150000003892 tartrate salts Chemical class 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
AGGKEGLBGGJEBZ-UHFFFAOYSA-N tetramethylenedisulfotetramine Chemical compound C1N(S2(=O)=O)CN3S(=O)(=O)N1CN2C3 AGGKEGLBGGJEBZ-UHFFFAOYSA-N 0.000 description 1
WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
238000011287 therapeutic dose Methods 0.000 description 1
230000004797 therapeutic response Effects 0.000 description 1
229960002898 threonine Drugs 0.000 description 1
239000003868 thrombin inhibitor Substances 0.000 description 1
239000003634 thrombocyte concentrate Substances 0.000 description 1
230000001732 thrombotic effect Effects 0.000 description 1
210000001519 tissue Anatomy 0.000 description 1
238000011200 topical administration Methods 0.000 description 1
FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
238000012546 transfer Methods 0.000 description 1
230000007704 transition Effects 0.000 description 1
238000013519 translation Methods 0.000 description 1
125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
125000004953 trihalomethyl group Chemical group 0.000 description 1
229960004799 tryptophan Drugs 0.000 description 1
229960004441 tyrosine Drugs 0.000 description 1
OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
230000002792 vascular Effects 0.000 description 1
235000015112 vegetable and seed oil Nutrition 0.000 description 1
239000008158 vegetable oil Substances 0.000 description 1
238000010792 warming Methods 0.000 description 1
238000005303 weighing Methods 0.000 description 1
UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
229940007718 zinc hydroxide Drugs 0.000 description 1
229910021511 zinc hydroxide Inorganic materials 0.000 description 1
ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Biochemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Animal Behavior & Ethology (AREA)
General Chemical & Material Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Diabetes (AREA)
Hematology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

SK146-99A 1996-08-21 1997-08-15 Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides SK14699A3 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US08/700,950 US5780590A (en)	1993-10-15	1996-08-21	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
PCT/US1997/014578 WO1998017678A1 (en)	1996-08-21	1997-08-15	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

Publications (1)

Publication Number	Publication Date
SK14699A3 true SK14699A3 (en)	2000-11-07

Family

ID=24815484

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK146-99A SK14699A3 (en)	1996-08-21	1997-08-15	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

Country Status (21)

Country	Link
US (1)	US5780590A (ru)
EP (1)	EP0929572A4 (ru)
JP (1)	JP2001501965A (ru)
KR (1)	KR20000035797A (ru)
CN (1)	CN1231671A (ru)
AP (1)	AP904A (ru)
AU (1)	AU722112B2 (ru)
BG (1)	BG103197A (ru)
BR (1)	BR9711205A (ru)
CA (1)	CA2263732A1 (ru)
EA (1)	EA001391B1 (ru)
HU (1)	HUP9903961A3 (ru)
IL (1)	IL128556A0 (ru)
NO (1)	NO990836L (ru)
NZ (1)	NZ334059A (ru)
OA (1)	OA10975A (ru)
PL (1)	PL331713A1 (ru)
SK (1)	SK14699A3 (ru)
UA (1)	UA48252C2 (ru)
WO (1)	WO1998017678A1 (ru)
ZA (1)	ZA977511B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6274705B1 (en)	1996-05-02	2001-08-14	Aventis Pharmaceuticals Products Inc.	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
CN1231659A (zh) *	1996-08-21	1999-10-13	罗纳·布朗克罗尔药制品有限公司	N[n－n－(4－哌啶－4－基)丁酰基)－n－乙基甘氨酰基]化合物的不吸湿的稳定结晶形式
WO1999019294A1 (en) *	1997-05-14	1999-04-22	Aventis Pharmaceuticals Products Inc. Legal/Patents	Process for the preparation of azacycloalkylalkanoyl pseudotetrapeptides
EP1030831A4 (en) *	1997-10-10	2003-01-02	Aventis Pharm Prod Inc	PREPARATION OF AZACYCLOALKYLALCANOYL PSEUDOTETRAPEPTIDES
WO2000040601A1 (en) *	1998-12-30	2000-07-13	Aventis Pharmaceuticals Products Inc.	Process for preparing a stable non-hygroscopic crystalline n-[n-[n- piperdin- 4-yl)butanoyl)- n.ethylglycyl]- (l)-aspartyl] -ss-cyclohexylalanine amide
US7200838B2 (en) *	2000-12-20	2007-04-03	National Instruments Corporation	System and method for automatically generating a graphical program in response to a state diagram
US7544681B2 (en)	2001-09-27	2009-06-09	Ramot At Tel Aviv University Ltd.	Conjugated psychotropic drugs and uses thereof
ES2400772T3 (es) *	2005-06-07	2013-04-12	Ramot At Tel Aviv University Ltd.	Sales novedosas de fármacos psicotrópicos conjugados y procedimientos para la preparación de las mismas
ES2393933T3 (es)	2006-07-17	2013-01-02	Ramot, At Tel Aviv University Ltd.	Conjugados que comprenden un fármaco psicotrópico o un agonista GABA y un ácido orgánico y su uso para el tratamiento del dolor y otros transtornos del SNC
US8207369B2 (en)	2008-02-11	2012-06-26	Ramot At Tel-Aviv University Ltd.	Conjugates for treating neurodegenerative diseases and disorders
EP2509603A1 (en)	2009-12-09	2012-10-17	Biolinerx Ltd.	Methods of improving cognitive functions
US8377929B2 (en)	2010-02-24	2013-02-19	Ramot At Tel-Aviv University Ltd.	Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
WO2012038963A1 (en)	2010-09-22	2012-03-29	Ramot At Tel-Aviv University Ltd.	An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same

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US3821188A (en) *	1972-06-14	1974-06-28	American Home Prod	Proline and pyroglutamic acid containing tripeptides
GB8600263D0 (en) *	1985-01-22	1986-02-12	Ici America Inc	Peptide derivatives
US4683291A (en) *	1985-10-28	1987-07-28	Scripps Clinic And Research Foundation	Platelet binding inhibitors
FR2608160B1 (fr) *	1986-12-15	1989-03-31	Inst Nat Sante Rech Med	Nouveaux derives peptidiques et leur application notamment en therapeutique
US4857508A (en) *	1987-12-03	1989-08-15	Monsanto Company	Novel platelet-aggregation inhibitor peptide derivatives
US4879313A (en) *	1988-07-20	1989-11-07	Mosanto Company	Novel platelet-aggregation inhibitors
US5037808A (en) *	1988-07-20	1991-08-06	Monsanto Co.	Indolyl platelet-aggregation inhibitors
US4992463A (en) *	1988-07-20	1991-02-12	Monsanto Company	Thienyl peptide mimetic compounds which are useful in inhibiting platelet aggregation
US5023233A (en) *	1989-07-28	1991-06-11	Merck & Co., Inc.	Fibrinogen receptor antagonists
EP0494248A4 (en) *	1989-09-29	1992-08-26	Rhone-Poulenc Rorer International (Holdings) Inc.	Anti-thrombotic peptides and pseudopeptides
US4952562A (en) *	1989-09-29	1990-08-28	Rorer Pharmaceutical Corporation	Anti-thrombotic peptides and pseudopeptides
US5051405A (en) *	1989-10-10	1991-09-24	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Anti-thrombotic peptides and pseudopeptides
US5053392A (en) *	1989-12-01	1991-10-01	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Novel arginine, glycine, aspartic acid derivatives as platelet-aggregation inhibitors
US5086069A (en) *	1990-02-05	1992-02-04	Rorer Pharmaceutical Corporation	Anti-thrombotic peptide and pseudopeptide derivatives
CA2037153A1 (en) *	1990-03-09	1991-09-10	Leo Alig	Acetic acid derivatives
GB9007751D0 (en) *	1990-04-05	1990-06-06	Ciba Geigy Ag	Novel platelet-aggregation inhibitors
US5064814A (en) *	1990-04-05	1991-11-12	Rhone-Poulenc Rorer Pharmaceuticals Inc.	Anti-thrombotic peptide and pseudopeptide derivatives
NZ239876A (en) *	1990-09-27	1993-12-23	Merck & Co Inc	Glycyl-b-alanine derivatives and pharmaceutical compositions thereof.
IL99539A0 (en) *	1990-09-27	1992-08-18	Merck & Co Inc	Fibrinogen receptor antagonists and pharmaceutical compositions containing them
MX9201416A (es) *	1991-03-28	1992-10-01	Rhone Poulenc Rorer Int	Peptidos y pseudopeptidos antitromboticos.
JPH08503920A (ja) *	1991-04-11	1996-04-30	ローヌ−プーランローラーインターナショナル（ホウルディングス）インコーポレイテッド	抗血栓ペプチドおよび偽ペプチド誘導体
DK0513675T3 (da) *	1991-05-13	1996-09-30	Fujisawa Pharmaceutical Co	Hidtil ukendt peptidforbindelse samt fremgangsmåde til fremstilling deraf
SK47796A3 (en) *	1993-10-15	1997-03-05	Rhone Poulenc Rorer Pharma	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

1996
- 1996-08-21 US US08/700,950 patent/US5780590A/en not_active Expired - Lifetime
1997
- 1997-08-15 CA CA002263732A patent/CA2263732A1/en not_active Abandoned
- 1997-08-15 IL IL12855697A patent/IL128556A0/xx unknown
- 1997-08-15 PL PL97331713A patent/PL331713A1/xx unknown
- 1997-08-15 EA EA199900216A patent/EA001391B1/ru not_active IP Right Cessation
- 1997-08-15 SK SK146-99A patent/SK14699A3/sk unknown
- 1997-08-15 AP APAP/P/1999/001452A patent/AP904A/en active
- 1997-08-15 UA UA99031553A patent/UA48252C2/ru unknown
- 1997-08-15 EP EP97938424A patent/EP0929572A4/en not_active Withdrawn
- 1997-08-15 BR BR9711205A patent/BR9711205A/pt not_active Application Discontinuation
- 1997-08-15 AU AU40749/97A patent/AU722112B2/en not_active Ceased
- 1997-08-15 NZ NZ334059A patent/NZ334059A/xx unknown
- 1997-08-15 JP JP10519340A patent/JP2001501965A/ja not_active Ceased
- 1997-08-15 KR KR1019997001363A patent/KR20000035797A/ko not_active Ceased
- 1997-08-15 CN CN97198164A patent/CN1231671A/zh active Pending
- 1997-08-15 HU HU9903961A patent/HUP9903961A3/hu unknown
- 1997-08-15 WO PCT/US1997/014578 patent/WO1998017678A1/en not_active Ceased
- 1997-08-21 ZA ZA9707511A patent/ZA977511B/xx unknown
1999
- 1999-02-15 OA OA9900033A patent/OA10975A/en unknown
- 1999-02-22 NO NO990836A patent/NO990836L/no unknown
- 1999-02-22 BG BG103197A patent/BG103197A/xx unknown

Also Published As

Publication number	Publication date
ZA977511B (en)	1998-03-03
HUP9903961A2 (hu)	2000-04-28
PL331713A1 (en)	1999-08-02
EA001391B1 (ru)	2001-02-26
EA199900216A1 (ru)	1999-08-26
HUP9903961A3 (en)	2000-12-28
BR9711205A (pt)	1999-08-17
US5780590A (en)	1998-07-14
KR20000035797A (ko)	2000-06-26
AP9901452A0 (en)	1999-03-31
JP2001501965A (ja)	2001-02-13
NO990836D0 (no)	1999-02-22
NO990836L (no)	1999-04-20
AP904A (en)	2000-11-24
CA2263732A1 (en)	1998-04-30
OA10975A (en)	2001-11-01
IL128556A0 (en)	2000-01-31
AU722112B2 (en)	2000-07-20
EP0929572A4 (en)	2001-09-12
BG103197A (bg)	2000-05-31
UA48252C2 (ru)	2002-08-15
CN1231671A (zh)	1999-10-13
AU4074997A (en)	1998-05-15
WO1998017678A1 (en)	1998-04-30
NZ334059A (en)	2000-01-28
EP0929572A1 (en)	1999-07-21

Publication	Publication Date	Title
US6153588A (en)	2000-11-28	Stable non-hygroscopic crystalline form of N-[N-[N-4-(piperidin-4-yl)butanoyl)-N-ethylglycyl] aspartyl]-L-β-cyclohexyl alanine amide
AP904A (en)	2000-11-24	Antithrombotic Azacycloalkylalkanoyl peptides and pseudopeptides.
RU2134695C1 (ru)	1999-08-20	Антитромботические азациклоалкилалканоилпептиды
CZ55099A3 (cs)	2000-06-14	Antitrombotické azacykloalkylalkanoylové peptidy a pseudopeptidy
US6274705B1 (en)	2001-08-14	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
MXPA99001773A (en)	1999-06-01	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
MXPA99001772A (en)	1999-06-01	Stable non-hygroscopic crystalline form of n-[n-n-(4-(piperidin-4-yl)butanoyl)-n-ethylglycyl]compounds
CZ55199A3 (cs)	2000-06-14	Stabilní, nehygroskopická krystalická forma N- [N-[N(4-piperidin-4-yl)butanoyl]-N-ethylgIycyl]ových derivátů
HK1022318A (en)	2000-08-04	Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
NZ299833A (en)	1998-04-27	Treating or preventing thrombosis using azacycloalkanol peptides and pseudopeptides